Chen, Yong; Wang, Xiaoyan; Xiang, Wei; He, Lin; Tang, Minghai; Wang, Fang; Wang, Taijin; Yang, Zhuang; Yi, Yuyao; Wang, Hairong; Niu, Ting; Zheng, Li; Lei, Lei; Li, Xiaobin; Song, Hang; Chen, Lijuan published the artcile< Development of Purine-Based Hydroxamic Acid Derivatives: Potent Histone Deacetylase Inhibitors with Marked in Vitro and in Vivo Antitumor Activities>, HPLC of Formula: 89793-12-4, the main research area is purine hydroxamic acid derivative preparation histone deacetylase inhibitor cancer.
In the present study, a series of novel histone deacetylase (HDAC) inhibitors using the morpholinopurine as the capping group were designed and synthesized. Several compounds demonstrated significant HDAC inhibitory activities and antiproliferative effects against diverse human tumor cell lines. Among them, compound 10o was identified as a potent class I and class IIb HDAC inhibitor with good pharmaceutical profile and druglike properties. Western blot anal. further confirmed that 10o more effectively increased acetylated histone H3 than panobinostat (LBH-589) and vorinostat (SAHA) at the same concentration in vitro. In in vivo efficacy evaluations of HCT116, MV4-11, Ramos, and MM1S xenograft models, 10o showed higher efficacy than SAHA or LBH-589 without causing significant loss of body weight and toxicity. All the results indicated that 10o could be a suitable candidate for treatment of both solid and hematol. cancer.
Journal of Medicinal Chemistry published new progress about Antitumor agents. 89793-12-4 belongs to class pyrimidines, and the molecular formula is C7H7ClN2O2, HPLC of Formula: 89793-12-4.
Referemce:
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia